Two University of Georgia College of Pharmacy faculty have received a patent for the invention of novel analogs of choline that may be used to treat neurodegenerative disorders.

Warren Beach, associate professor in the department of pharmaceutical and biomedical sciences, and Alvin Terry, professor in the department of clinical and administrative pharmacy, in collaboration with Jerry Buccafusco, director of the Alzheimer Research Center at the Medical College of Georgia, are developing novel compounds against such diseases as Alzheimer's, Parkinson's, Huntington's and related disorders.

Compounds according to the present invention are effective to alleviate and/or reverse the effects of a neurodegenerative condition, prevent further deterioration and/or enhance cognition and memory in patients suffering from neurodegenerative disorders, especially Alzheimer's disease.

"The new choline analogs are potentially useful in the treatment of any neurological condition where acetylcholine transmission neurons [cholinergic neurons] are affected," said Beach. These cholinergic neurons are involved in cognitive functions, such as learning and memory, and Alzheimer's disease is characterized by a loss of these neurons.

Currently, Beach noted, the primary treatment of Alzheimer's is acetylcholine esterase inhibitors that inhibit the breakdown of acetylcholine in the brain, thus enhancing cholinergic transmission. Choline, the breakdown product of acetylcholine, has been shown to be protective against cell death. This protection arises through choline's stimulation of a receptor called Alpha 7 that is located on the acetylcholine neuron.

"Choline has been evaluated as a treatment of Alzheimer's disease, however choline is not very potent and shows poor oral absorption. Several of our choline analogs are approximately 100,000 times more potent than choline in cell culture and should have better absorption characteristics and brain penetration than choline," said Beach.

Source: Eurekalert & others

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By John M. Grohol, Psy.D. on
21 Feb 2009
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